Article ID Journal Published Year Pages File Type
10593024 Bioorganic & Medicinal Chemistry Letters 2013 8 Pages PDF
Abstract
A series of novel tri-2,3,5-substituted tetrahydropyran analogs were synthesized and evaluated as inhibitors of dipeptidyl peptidase 4 (DPP-4) for the treatment of type 2 diabetes. Optimization of the series provided inhibitors with good DPP-4 potency and selectivity over other peptidases (QPP, DPP8, and FAP). Compound 23, which is very potent, selective, efficacious in the diabetes PD model, and has an excellent pharmacokinetic profile, is selected as a clinical candidate.
Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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